Activators & Inhibitors

HIV-1 inhibitor-31 (compound 4) is a potent inhibitor of HIV-1. HIV-1 inhibitor-31 can be used in the study of AIDS.

VEGFR-2-IN-16 (Compound 15b) is a potent inhibitor of VEGFR-2 (IC50: 86.36 nM) that exhibits antitumour effects.

HDAC-IN-47 is an orally active histone deacetylase (HDAC) inhibitor with IC50 values of 19.75 nM, 57.8 nM, 40.27 nM, 5.63 nM and 302.73 nM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8, respectively. HDAC-IN-47 can block the cell cycle in G2/M phase, inhibit autophagy, induce apoptosis using the Bax/Bcl-2 and caspase-3 pathways, and has anti-cancer activity in vivo.

PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor that exhibits anticancer effects without toxicity to normal cells. PI3Kα-IN-6 increases ROS production, decreases mitochondrial membrane potential and induces apoptosis.

MYF-03-176 is an orally active anticancer agent. MYF-03-176 exhibits strong antitumour effects in the MPM mouse xenograft tumour model following oral administration.

HSV-1/HSV-2-IN-1 is an HSV-1 and HSV-2 inhibitor that acts against HSV-1 (KOS) (EC50: 7.6 μM), HSV-2 (G) (EC50: 7.6 μM), HSV-1 TK-KOS ACVr (EC50: 4 μM) and cowpox virus (EC50: 12 μM).

LPM4870108 is a potent, orally active pan-Trk (WT/MT) inhibitor that acts on TrkC (IC50: 0.2 nM), TrkA (IC50: 2.4 nM), TrkAG595R (IC50: 3.5 nM) and TrkAG667C (IC50: 2.3 nM), and is more selective for Trk than ALK (IC50: 2.3 nM). LPM4870108 showed anti-tumour effects.

VT103 is an orally active and selective inhibitor of TEAD1 protein palmitoylation and is an analog of VT101. VT103 has potential antitumor activity by inhibiting YAP/TAZ-TEAD-promoted gene transcriptionment, blocking TEAD auto-palmitoylation, and blocking the interaction between YAP/TAZ and TEAD.VT103 can be used in the study of HER2-positive breast cancer, prostate cancer, and triple-negative breast cancer.

Akt/NF-κB/JNK-IN-1 (Compound 2i) is an inhibitor of Akt, NF-κB and JNK signalling pathways.Akt/NF-κB/JNK-IN-1 exhibits an inhibitory effect on nitric oxide production (IC50: 3.15 μM) and shows anti-inflammatory effects.